In the present study, novel derivatives of 4H-benzo[h]chromene and 7H-benzo[h]chromeno[2,3-d]pyrimidine were prepared and evaluated for their anti-proliferative activity against three human tumor cell lines breast adenocarcinoma (MCF-7), human colon carcinoma (HCT-116) and hepatocellular carcinoma (HepG-2) in comparison with the standard drugs Doxorubicin, Vinblastine and Colchicine using MTT colorimetric assay. The structures of the target compounds were established on the basis of spectral data. We explored the Structure–Activity Relationship (SAR) of 4H-benzo[h]chromenes with modification at the 2- or 3- and 2, 3-positions. It was found that several compounds showed good antitumor activity against the cell lines MCF-7, HCT-116 and HepG-2 as compared to the standard drugs. The SAR study revealed that the antitumor activity of the synthesized compounds was significantly affected by the lipophilicity (hydrophobic or hydrophilic) of the substituent at 2- or 3- and 2, 3-positions.
El-Agrody, A. M., Halawa, A. H., Fouda, A. M., & Al-Dies, A. A. M. (2017). The anti-proliferative activity of novel 4H-benzo[h]chromenes, 7H-benzo[h]-chromeno[2,3-d]pyrimidines and the structure–activity relationships of the 2-, 3-positions and fused rings at the 2, 3-positions. Journal of Saudi Chemical Society, 21(1), 82–90. https://doi.org/10.1016/j.jscs.2016.03.002